公开(公告)号：US20200306247A1

公开(公告)日：2020-10-01

申请号：US16903133

申请日：2020-06-16

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert DAVIS

IPC: A61K31/4985 ,  A61K9/48 ,  A61K9/00 ,  A61K9/16

Abstract: The present disclosure relates to pharmaceutical capsules comprising lumateperone, in free, or pharmaceutically acceptable salt form, optionally in combination with one or more additional therapeutic agents, processes for manufacture thereof and methods of use in the treatment or prophylaxis of disease.

公开(公告)号：US20190298730A1

公开(公告)日：2019-10-03

申请号：US16443240

申请日：2019-06-17

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Kimberly VANOVER ,  Peng LI ,  Sharon MATES ,  Robert DAVIS ,  Lawrence P. WENNOGLE

IPC: A61K31/5383 ,  A61K31/4985 ,  A61K9/00 ,  A61K45/06 ,  A61K9/51

Abstract: The disclosure provides the use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of residual symptoms of psychosis or schizophrenia. The disclosure also provides novel long acting injectable formulations of particular substituted heterocycle fused gamma-carboline compounds and use of such long acting injectable formulations for the treatment of residual symptoms of psychosis or schizophrenia.

公开(公告)号：US20180200256A1

公开(公告)日：2018-07-19

申请号：US15918955

申请日：2018-03-12

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Kimberly VANOVER ,  Peng LI ,  Sharon MATES ,  Robert DAVIS ,  Lawrence P. WENNOGLE

IPC: A61K31/5383 ,  A61K9/00 ,  A61K9/51 ,  A61K45/06 ,  A61K31/4985

CPC classification number: A61K31/5383 ,  A61K9/0019 ,  A61K9/0024 ,  A61K9/5153 ,  A61K31/4985 ,  A61K45/06 ,  A61K2300/00

Abstract: The disclosure provides the use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of residual symptoms of psychosis or schizophrenia. The disclosure also provides novel long acting injectable formulations of particular substituted heterocycle fused gamma-carboline compounds and use of such long acting injectable formulations for the treatment of residual symptoms of psychosis or schizophrenia.

公开(公告)号：US20170283417A1

公开(公告)日：2017-10-05

申请号：US15629481

申请日：2017-06-21

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Qiang ZHANG ,  Robert DAVIS ,  Lawrence P. Wennogle

IPC: C07D471/16 ,  A61K9/48 ,  A61K9/50 ,  A61K31/4985 ,  A61K47/38 ,  C07D471/14 ,  A61K47/34

CPC classification number: C07D471/16 ,  A61K9/4825 ,  A61K9/4891 ,  A61K9/5031 ,  A61K31/4985 ,  A61K47/34 ,  A61K47/38 ,  C07D471/14

Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D2 receptor signaling systems.

公开(公告)号：US20240216368A1

公开(公告)日：2024-07-04

申请号：US18602981

申请日：2024-03-12

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert DAVIS

IPC: A61K31/4985 ,  A61K9/00 ,  A61K9/16 ,  A61K9/48

CPC classification number: A61K31/4985 ,  A61K9/0053 ,  A61K9/16 ,  A61K9/4825 ,  A61K9/485 ,  A61K9/4858 ,  A61K9/4891

Abstract: The present disclosure relates to pharmaceutical capsules comprising lumateperone, in free, or pharmaceutically acceptable salt form, optionally in combination with one or more additional therapeutic agents, processes for manufacture thereof and methods of use in the treatment or prophylaxis of disease.

公开(公告)号：US20240016802A1

公开(公告)日：2024-01-18

申请号：US18476138

申请日：2023-09-27

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Wei YAO ,  Robert DAVIS

IPC: A61K31/4985 ,  A61K9/06 ,  A61K9/00

CPC classification number: A61K31/4985 ,  A61K9/06 ,  A61K9/006 ,  A61K9/0043 ,  A61K9/0036

Abstract: The disclosure provides new transmucosal and subcutaneous pharmaceutical compositions comprising 1-(4-fluoro-phenyl)-4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3′,4′:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one or 1-(4-fluoro-phenyl)-4-((6bR,10aS)-2,2-d2-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3′,4′:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one or comprising -(4-fluoro-phenyl)-4-((6bR,10aS)-1,1,2,2-d4-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3′,4′:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one, in free base, co-crystal or salt form, together with methods of making and using them.

公开(公告)号：US20240009195A1

公开(公告)日：2024-01-11

申请号：US18007018

申请日：2021-07-26

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  David KASS ,  Robert DAVIS ,  Gretchen SNYDER

IPC: A61K31/519 ,  A61K31/7034 ,  A61K45/06 ,  A61P9/04

CPC classification number: A61K31/519 ,  A61K31/7034 ,  A61K45/06 ,  A61P9/04

Abstract: The disclosure provides methods, treatments and materials for treating diseases or disorders mediated by cyclic nucleotides and/or sodium glucose cotransporter 2. In particular, the present disclosure provides for methods of treating such diseases and disorders with a PDE1 inhibitor in combination with additional therapeutic agents.

公开(公告)号：US20230301995A1

公开(公告)日：2023-09-28

申请号：US18319425

申请日：2023-05-17

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Wei YAO ,  Robert DAVIS

IPC: A61K31/4985 ,  A61K9/06 ,  A61K9/00

CPC classification number: A61K31/4985 ,  A61K9/06 ,  A61K9/006 ,  A61K9/0043 ,  A61K9/0036

Abstract: The disclosure provides new transmucosal and subcutaneous pharmaceutical compositions comprising 1-(4-fluoro-phenyl)-4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3′,4′:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one or 1-(4-fluoro-phenyl)-4-((6bR,10aS)-2,2-d2-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3′,4′:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one or comprising -(4-fluoro-phenyl)-4-((6bR,10aS)-1,1,2,2-d4-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3′,4′:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one, in free base, co-crystal or salt form, together with methods of making and using them.

公开(公告)号：US20230203037A1

公开(公告)日：2023-06-29

申请号：US18067387

申请日：2022-12-16

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon MATES ,  Peng LI ,  Lawrence P. WENNOGLE ,  Robert DAVIS

IPC: C07D471/16 ,  C07D471/14 ,  A61K45/06 ,  C07B59/00 ,  A61P25/24 ,  A61P25/22 ,  A61P25/18 ,  A61K31/4985

CPC classification number: C07D471/16 ,  C07D471/14 ,  A61K45/06 ,  C07B59/002 ,  A61P25/24 ,  A61P25/22 ,  A61P25/18 ,  A61K31/4985

Abstract: This invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D1/D2 receptor signaling systems, and/or the treatment of residual symptoms.

公开(公告)号：US20220296591A1

公开(公告)日：2022-09-22

申请号：US17832282

申请日：2022-06-03

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Wei YAO ,  Robert DAVIS ,  Sharon MATES ,  Kimberly VANOVER ,  Gretchen SNYDER

IPC: A61K31/4985 ,  A61P25/36 ,  A61P23/00 ,  A61K9/00 ,  A61K9/16 ,  A61K31/137 ,  A61K31/485 ,  A61K45/06

Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and/or the μ-opioid receptor.